非典型该项受体3 t3-f442a脂肪细胞。药理和分子与人类β3-adrenergic受体的关系。
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Feve B, Emorine LJ, Lasnier F,俄式薄煎饼N, Baude B, C纳米亚斯,Strosberg广告,Pairault J
非典型该项受体3 t3-f442a脂肪细胞。药理和分子与人类β3-adrenergic受体的关系。
J生物化学杂志。1991年10月25日,266 (30):20329 - 36。
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1682311 (在PubMed]
- 文摘
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表现为非典型该项受体配体结合的属性(beta-AR)亚型进行了研究在小鼠的脂肪分化3 t3-f442a细胞并与人类β3-AR表示在中国仓鼠卵巢细胞稳定转染与人类β3-AR基因(CHO-beta 3细胞)Emorine l . J。、Marullo年代。Briend-Sutren, M . M。,帕蒂,他步行G。泰特,K。Delavier-Klutchko C。Strosberg,公元245年(1989年)科学,1118 - 1121)。3 t3-f442a脂肪细胞表现出高和低亲和力结合位点(-)4 - (3-t-butylamino-2-hydroxypropoxy) [5, 7-3H] benzimidazole-2-one ((-) - [3 h]本金保证产品- 12177)(KD = 1.2和38.3 nM)和(-)- [125 i] iodocyanopindolol ([125 i] CYP) (KD = 47和1510点)。高亲和力的网站与经典的β1 -和β2-AR亚型而KD值的低放射性配体的亲和力网站类似以CHO-beta 3细胞(KD = 28 nM和1890点(-)- [3 h] CGP12177 [125 i] CYP,分别)。这些低亲和力网站在preadipocytes已经察觉,但约占总额的90% beta-ARs脂肪细胞。非典型beta-AR和人类β3-AR添加类似的低亲和力(Ki = 3 - 5 microM) (+ / -) - (2 - (3-carbamoyl-4-hydroxyphenoxy) ethylamino-3) - (4 - (1 - 4 - trifluormethyl-2-imidazolyl)苯氧基)丙胺甲烷磺酸盐(CGP20712A)或erythro - (+ / -) 1 - (7-methylindan-4-yloxy) 3-isopropylaminob utan-2-ol (ICI118551),高选择性β1 -和β2-AR拮抗剂,分别符合穷人的抑制作用的化合物(-)异丙肾上腺素(IPR)刺激腺苷酸环化酶的活动。非典型beta-AR和β3-AR有亲和力的10 - 50倍sodium-4 - (2 - [2-hydroxy-2 - (3-chlorophenyl) ethylamino]丙)phenoxyace泰特sesquihydrate比β1-AR亚型(BRL37344)。这与有效BRL37344脂肪细胞的脂解的影响。 The rank order of potency of agonists in functional and binding studies was BRL37344 greater than IPR less than (-)-norepinephrine greater than (-)-epinephrine both in 3T3 adipocytes and CHO-beta 3 cells. As in CHO-beta 3 cells, the classical beta 1- and beta 2-antagonists CGP12177, oxprenolol, and pindolol were partial agonists in adipocytes. Although undetectable in preadipocytes, a major mRNA species of 2.3 kilobases (kb) and a minor one of 2.8 kb were observed in adipocytes by hybridization to a human beta 3-AR specific probe.(ABSTRACT TRUNCATED AT 400 WORDS)